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CO5700818A2 - OXAZOL TETRACICLINE DERIVATIVES - Google Patents

OXAZOL TETRACICLINE DERIVATIVES

Info

Publication number
CO5700818A2
CO5700818A2 CO06055450A CO06055450A CO5700818A2 CO 5700818 A2 CO5700818 A2 CO 5700818A2 CO 06055450 A CO06055450 A CO 06055450A CO 06055450 A CO06055450 A CO 06055450A CO 5700818 A2 CO5700818 A2 CO 5700818A2
Authority
CO
Colombia
Prior art keywords
optionally substituted
carbon atoms
substituted carbon
alkyl
atoms
Prior art date
Application number
CO06055450A
Other languages
Spanish (es)
Inventor
Phaik-Eng Sum
David Brian How
Darrin William Hopper
Matthew Douglas Vera
Joshua James Sabatini
Original Assignee
Wyeth Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34681543&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO5700818(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of CO5700818A2 publication Critical patent/CO5700818A2/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/62Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems having two or more ring systems containing condensed 1,3-oxazole rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/65Tetracyclines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/40Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/461,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

De acuerdo con la presente invención, se suministran compuestos representados por la Fórmula (I); En donde: X se selecciona del grupo hidrógeno, amino, NR11R12, alquilo de 1 a 12 átomos de carbono opcionalmente sustituido, arilo de 6, 10 o 14 átomos de carbono opcionalmente sustituido, vinilo opcionalmente sustituido, alquinilo de 2 a 12 átomos de carbono opcionalmente sustituido y halógeno;A" es una porción seleccionada del grupo: R11 y R12 son cada uno independientemente H o alquilo de 1 a 12 átomos de carbono o R11 y R12 cuando se toman opcionalmente juntos con el átomo de nitrógeno al cual cada uno está unido forman un anillo de hidrocarburo saturado de 3 a 7 miembros; Y se selecciona de hidrógeno, alquilo de 1 a 12 átomos de carbono opcionalmente sustituido, arilo de 6, 10 o 14 átomos de carbono opcionalmente sustituido, alquenilo de 2 a 12 átomos de carbono opcionalmente sustituido, vinilo, alquinilo de 2 a 12 átomos de carbono opcionalmente sustituido y halógeno;R se selecciona de alquilo de 1 a 12 átomos de carbono opcionalmente sustituido, alquenilo de 2 a 12 átomos de carbono opcionalmente sustituido, alquinilo de 2 a 12 átomos de carbono opcionalmente sustituido, -CH2NR1R2, arilo de 6, 10 o 14 átomos de carbono opcionalmente sustituido, aralquilo de 7 a 16 átomos de carbono opcionalmente sustituido, aroilo de 7 a 13 átomos de carbono opcionalmente sustituido, SR3, heteroarilo de 5 o 6 átomos por anillo opcionalmente sustituido, que contiene 1 a 4 heteroátomos que pueden ser iguales o diferentes, independientemente seleccionados de nitrógeno, oxígeno y azufre, y heteroarilcarbonilo de 5 o 6 átomos por anillo opcionalmente sustituido que contiene 1 a 4 heteroátomos que pueden ser iguales o diferentes, independientemente seleccionados de nitrógeno, oxígeno y azufre; ...In accordance with the present invention, compounds represented by Formula (I) are supplied; Where: X is selected from the group hydrogen, amino, NR11R12, alkyl of 1 to 12 optionally substituted carbon atoms, aryl of 6, 10 or 14 optionally substituted carbon atoms, optionally substituted vinyl, alkynyl of 2 to 12 carbon atoms optionally substituted and halogen; A "is a portion selected from the group: R11 and R12 are each independently H or alkyl of 1 to 12 carbon atoms or R11 and R12 when optionally taken together with the nitrogen atom to which each is attached form a 3 to 7-membered saturated hydrocarbon ring; and is selected from hydrogen, optionally substituted alkyl of 1 to 12 carbon atoms, optionally substituted aryl of 6, 10 or 14 carbon atoms, alkenyl of 2 to 12 atoms of optionally substituted carbon, vinyl, alkynyl of 2 to 12 optionally substituted carbon atoms and halogen; R is selected from alkyl of 1 to 12 optionally substituted carbon atoms, alkenyl of 2 to 12 optionally substituted carbon atoms, alkynyl of 2 to 12 optionally substituted carbon atoms, -CH2NR1R2, aryl of 6, 10 or 14 optionally substituted carbon atoms, aralkyl of 7 to 16 optionally substituted carbon atoms, aroyl of 7 to 13 optionally substituted carbon atoms, SR3, heteroaryl of 5 or 6 atoms per optionally substituted ring, containing 1 to 4 heteroatoms that may be the same or different, independently selected from nitrogen, oxygen and sulfur, and heteroarylcarbonyl of 5 or 6 atoms per ring optionally substituted containing 1 to 4 heteroatoms that may be the same or different, independently selected from nitrogen, oxygen and sulfur; ...

CO06055450A 2003-12-08 2006-06-08 OXAZOL TETRACICLINE DERIVATIVES CO5700818A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US52792803P 2003-12-08 2003-12-08
US58482304P 2004-07-01 2004-07-01

Publications (1)

Publication Number Publication Date
CO5700818A2 true CO5700818A2 (en) 2006-11-30

Family

ID=34681543

Family Applications (1)

Application Number Title Priority Date Filing Date
CO06055450A CO5700818A2 (en) 2003-12-08 2006-06-08 OXAZOL TETRACICLINE DERIVATIVES

Country Status (25)

Country Link
US (3) US7176225B2 (en)
EP (2) EP2157085B1 (en)
JP (1) JP4848287B2 (en)
KR (1) KR101164262B1 (en)
CN (1) CN100545151C (en)
AR (1) AR047274A1 (en)
AT (2) ATE444290T1 (en)
AU (1) AU2004297243B2 (en)
BR (1) BRPI0417421A (en)
CA (1) CA2546895A1 (en)
CO (1) CO5700818A2 (en)
CR (1) CR8437A (en)
DE (1) DE602004023417D1 (en)
EC (1) ECSP066605A (en)
ES (2) ES2372635T3 (en)
IL (2) IL176162A (en)
MY (1) MY146098A (en)
NO (1) NO20062629L (en)
PA (1) PA8619601A1 (en)
PE (1) PE20050995A1 (en)
RU (1) RU2415844C2 (en)
SG (1) SG148216A1 (en)
TW (1) TW200528437A (en)
UA (2) UA83266C2 (en)
WO (1) WO2005056538A1 (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT1753713T (en) 2004-05-21 2016-11-25 President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
EP1805134B1 (en) 2004-10-25 2012-06-20 Paratek Pharmaceuticals, Inc. 4-aminotetracyclines and methods of use thereof
AR057033A1 (en) * 2005-05-27 2007-11-14 Wyeth Corp TIGECICLINE AND METHODS TO PREPARE 9-NITROMINOCICLINE
AR057324A1 (en) * 2005-05-27 2007-11-28 Wyeth Corp TIGECICLINE AND METHODS TO PREPARE 9-AMINOMINOCICLINE
AR057032A1 (en) * 2005-05-27 2007-11-14 Wyeth Corp TIGECICLINE AND PREPARATION METHODS
WO2007014154A2 (en) * 2005-07-21 2007-02-01 Paratek Pharmaceuticals, Inc. 10-substituted tetracyclines and methods of use thereof
US8486921B2 (en) 2006-04-07 2013-07-16 President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
EP2487160B1 (en) 2006-10-11 2016-02-03 President and Fellows of Harvard College Synthesis of Enone Intermediate
WO2008045507A2 (en) 2006-10-11 2008-04-17 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of bacillus anthracis infections
US8121767B2 (en) * 2007-11-02 2012-02-21 GM Global Technology Operations LLC Predicted and immediate output torque control architecture for a hybrid powertrain system
US8252946B2 (en) 2007-11-14 2012-08-28 Sandoz Ag Crystalline forms of tigecycline hydrochloride
US8338477B2 (en) 2008-07-11 2012-12-25 Neumedics Tetracycline derivatives with reduced antibiotic activity and neuroprotective benefits
SI2376433T1 (en) 2008-12-18 2015-03-31 Sandoz Ag Crystalline form c of tigecycline dihydrochloride and methods for its preparation
US9073829B2 (en) 2009-04-30 2015-07-07 President And Fellows Of Harvard College Synthesis of tetracyclines and intermediates thereto

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US26253A (en) * 1859-11-29 Vegetable-cutter
US2482055A (en) 1948-02-11 1949-09-13 American Cyanamid Co Aureomycin and preparation of same
US3007965A (en) 1959-02-13 1961-11-07 American Cyanamid Co New tetracyclines produced by streptomyces aureofaciens
US3043875A (en) 1959-10-22 1962-07-10 Pfizer & Co C Halogenated tetracycline derivatives and processes for their preparation
FR1430859A (en) 1960-05-23 1966-05-25
US3338963A (en) 1960-10-28 1967-08-29 American Cyanamid Co Tetracycline compounds
US3148212A (en) 1961-12-22 1964-09-08 American Cyanamid Co Reductive alkylation process
US3360557A (en) 1963-05-10 1967-12-26 American Cyanamid Co 9-hydroxytetracyclines and a process of preparing same
USRE26253E (en) 1963-05-17 1967-08-15 And z-alkylamino-g-deoxytetracycline
US3341585A (en) 1966-05-06 1967-09-12 American Cyanamid Co Substituted 7-and/or 9-amino-6-deoxytetracyclines
US3360561A (en) 1967-06-19 1967-12-26 American Cyanamid Co Nitration of tetracyclines
US3518306A (en) 1968-02-19 1970-06-30 American Cyanamid Co 7- and/or 9-(n-nitrosoalkylamino)-6-demethyl-6-deoxytetracyclines
US4806529A (en) 1982-11-18 1989-02-21 Trustees Of Tufts College, Tufts University Tetracycline activity enhancement
US5494903A (en) * 1991-10-04 1996-02-27 American Cyanamid Company 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
DE122006000058I1 (en) * 1991-10-04 2007-01-18 Wyeth Corp 7-Substituted-9-substituted-amino-6-demethyl-6-deoxy-tetracyclines
US5328902A (en) 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
WO2001010385A2 (en) * 1999-08-10 2001-02-15 Smithkline Beecham Corporation 1,4-substituted 4,4-diaryl cyclohexanes
EP2301550A1 (en) * 2001-07-13 2011-03-30 Paratek Pharmaceuticals, Inc. Tetracycline compounds having target therapeutic activities

Also Published As

Publication number Publication date
IL176162A0 (en) 2006-10-05
IL206050A (en) 2013-01-31
BRPI0417421A (en) 2007-03-13
US20080177080A1 (en) 2008-07-24
ES2372635T3 (en) 2012-01-25
KR101164262B1 (en) 2012-07-09
RU2006118367A (en) 2008-01-20
IL176162A (en) 2011-09-27
US20050153944A1 (en) 2005-07-14
EP1692117B1 (en) 2009-09-30
US20080064667A1 (en) 2008-03-13
RU2415844C2 (en) 2011-04-10
MY146098A (en) 2012-06-29
SG148216A1 (en) 2008-12-31
PE20050995A1 (en) 2006-01-11
UA83266C2 (en) 2008-06-25
ATE444290T1 (en) 2009-10-15
CN100545151C (en) 2009-09-30
CA2546895A1 (en) 2005-06-23
EP2157085A1 (en) 2010-02-24
CR8437A (en) 2006-10-06
WO2005056538A1 (en) 2005-06-23
AU2004297243B2 (en) 2011-02-17
US7365087B2 (en) 2008-04-29
CN1890226A (en) 2007-01-03
AU2004297243A1 (en) 2005-06-23
KR20060105047A (en) 2006-10-09
IL206050A0 (en) 2010-11-30
NO20062629L (en) 2006-09-06
EP2157085B1 (en) 2011-09-21
JP2007515411A (en) 2007-06-14
UA83268C2 (en) 2008-06-25
JP4848287B2 (en) 2011-12-28
TW200528437A (en) 2005-09-01
US7176225B2 (en) 2007-02-13
EP1692117A1 (en) 2006-08-23
DE602004023417D1 (en) 2009-11-12
AR047274A1 (en) 2006-01-11
ECSP066605A (en) 2006-10-25
ES2331574T3 (en) 2010-01-08
ATE525365T1 (en) 2011-10-15
PA8619601A1 (en) 2006-03-24

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